粉防己碱固体脂质纳米粒的制备

Li Ying-chao, Dong Lei, Jia Ai, Chang Xin-ming, Xue Hui

Department of Gastroenterology, First Affiliated Hospital, Medical College, Xi'an Jiaotong University, Xi'an 710061, China.

Zhongguo Yi Xue Ke Xue Yuan Xue Bao. 2006 Oct;28(5):686-9.

OBJECTIVE

To prepare solid lipid nanoparticles (SLN) loaded tetrandrine (TET) extracted from traditional Chinese medicine with ultrasonication and high pressure homogenization, and to compare the physicochemical characteristics of the particles produced by the two methods.

METHODS

TET was incorporated into SLN by ultrasonication and high pressure homogenization separately. Transmission electron microscopy was employed to study the shape. Particle characterization system and Zeta potential analyzer were used to study the diameter and Zeta potential of SLN in suspension. The entrapment efficiency was determined with the high-performance liquid chromatography. The stability of SLN was also studied.

RESULTS

TET-SLNs prepared by these two methods were sheet-shaped and irregular, but the SLNs prepared by high pressure homogenization were smaller. The mean diameter of SLN prepared by ultrasonication was (92 +/- 6) nm with Zeta potential of (-21.11 +/- 2.12) mV in distilled water, and the mean entrapment efficiency was 95.27%. The mean diameter of TET-SLN prepared by high pressure homogenization was (47 +/- 3) nm with Zeta potential of (-32.99 +/- 2.54) mV, and up to 97.82% of TET was incorporated. The diameter of SLN prepared by high pressure homogenization and ultrasonication were (52 +/- 5) nm and (168 +/- 12) nm after 90 days of storage at room temperature.

CONCLUSION

Compared with ultrasonication, high pressure homogenization is a better method to prepare TET-SLN, which is smaller, steadier and highly incorporated.

目的

采用超声法和高压均质法制备载有从中药中提取的粉防己碱（TET）的固体脂质纳米粒（SLN），并比较两种方法制备的颗粒的理化特性。

方法

分别通过超声法和高压均质法将TET载入SLN。采用透射电子显微镜研究其形态。用颗粒表征系统和Zeta电位分析仪研究悬浮液中SLN的直径和Zeta电位。用高效液相色谱法测定包封率。还研究了SLN的稳定性。

结果

两种方法制备的TET-SLN均为片状且不规则，但高压均质法制备的SLN较小。超声法制备的SLN在蒸馏水中的平均直径为（92±6）nm，Zeta电位为（-21.11±2.12）mV，平均包封率为95.27%。高压均质法制备的TET-SLN平均直径为（47±3）nm，Zeta电位为（-32.99±2.54）mV，TET的载入率高达97.82%。在室温下储存90天后，高压均质法和超声法制备的SLN直径分别为（52±5）nm和（168±12）nm。